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Cat. No. Product Name CAS No. Information
PC-43511

Capmatinib

1029712-80-8

Capmatinib (INCB-28060, INC-280) is a highly potent, selective, ATP competitive inhibitor of c-MET kinase with IC50 of 0.13 nM, displays no activity against RONβ, EGFR and HER-3; inhibits c-MET phosphorylation (IC50=1 nM) in SNU-5 human gastric cancer cell line, is slightly more potent in H596 and H1437 lung cancer cell lines that express mutant c-MET due to an exon 14 deletion and a R988C mutation; inhibits c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models.

Lung Cancer

Phase 3 Clinical

PC-43478

MK-8033 hydrochloride

1283000-43-0

MK-8033 is a potent, specific, dual c-Met/Ron kinases inhibitor with IC50 of 1/7 nM, also potently inhibits oncogenic c-Met activation loop mutants Y1230C, Y1230H and Y1235D with IC50 of 0.6-1.2 nM; MK-8033 is >100-fold selective relative to Ron and c-Met inhibition against a panel of 221 kinases; potently and selectively inhibits growth in c-Met amplified cell lines (GTL-16 proliferation IC50 =582 nM), causes full inhibition of tumor growth in c-Met amplified (GTL-16) subcutaneous tumor xenograft model; synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth.

Solid Tumors

Phase 1 Clinical

PC-43477

MK-8033

1001917-37-8

MK-8033 is a potent, specific, dual c-Met/Ron kinases inhibitor with IC50 of 1/7 nM, also potently inhibits oncogenic c-Met activation loop mutants Y1230C, Y1230H and Y1235D with IC50 of 0.6-1.2 nM; MK-8033 is >100-fold selective relative to Ron and c-Met inhibition against a panel of 221 kinases; potently and selectively inhibits growth in c-Met amplified cell lines (GTL-16 proliferation IC50 =582 nM), causes full inhibition of tumor growth in c-Met amplified (GTL-16) subcutaneous tumor xenograft model; synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth.

Solid Tumors

Phase 1 Clinical

PC-42888

BMS 777607

1025720-94-8

BMS 777607 is a potent, selective, orally efficacious inhibitor of Met kinase with IC50 of 3.9 nM, also potently inhibits Ron, Axl, Tyro-3 and Mer (IC50<15 nM), 40-fold selectivity over Lck, VEGFR-2 and TrkA/B; inhibits cell scattering activated by exogenous HGF in c-Met-expressing PC-3 and DU145 prostate cancer cells, suppresses HGF-stimulated cell migration and invasion with IC50 of <0.1 uM; potently blocks HGF-stimulated c-Met autophosphorylation and downstream activation of Akt and ERK at nanomolar level; demonstrates complete tumor stasis in Met-dependent GTL-16 human gastric carcinoma xenograft models.

Gastric Cancer

Phase 2 Clinical

PC-70080

Glesatinib

936694-12-1

Glesatinib (MGCD-265) is a tyrosine kinase inhibitor that potently and selectively inhibits Met and Axl kinase.

Lung Cancer

Phase 2 Clinical

PC-60074

Glumetinib

1642581-63-2

Glumetinib (SCC 244) is a novel potent and highly selective inhibitor of c-Met kinase with IC50 of 0.42 nM; displays high selectivity versus 312 other tested protein kinases; profoundly and specifically inhibits c-Met signal transduction and suppresses the c-Met-dependent neoplastic phenotype of tumor and endothelial cells; exhibits robust in vivo antitumor activity in NSCLC and hepatocellular carcinoma models.

Lung Cancer

Preclinical

PC-45842

Tivantinib

905854-02-6

Tivantinib (ARQ-197) is a potent, selective, non-ATP-competitive inhibitor of c-Met with Ki of 355 nM; has no inhibition for EGFR, InsR, PDGFRα, FGFR1 and FGFR4 etc., only modest inhibition (35%) for Ron at 30 uM; inhibits constitutive c-Met phosphorylation in HT29 and MKN-45 cells, and HGF-induced c-Met phosphorylation in MDA-MB-231 and NCI-H441 cells with IC50 of 100-300 nM; shows antiproliferative activity against multiple cancer cell lines (IC50=0.03-30 uM); exerts tumor growth inhibition in multiple mouse xenograft; orally active.

Liver Cancer

Phase 3 Clinical

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